Classes
Class | Examples | Description |
---|---|---|
Nucleoside reverse-transcriptase inhibitor (NRTI) | tenofovir, emtricitabine, abacavir | Nucleoside/nucleotide analogues that get incorporated into viral DNA by reverse transcriptase, causing missense or non-sense mutations. The backbone of HIV treatments, with a high barrier to resistance. |
Non-NRTI | efavirenz | Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation. |
Protease inhibitor (PI) | dirunavir | Inhibits protease, which is required for processing proteins in the creation of the virion. Causes a metabolic syndrome. |
Integrase strand transfer inhibitor (INSTI) | raltegravir, dolutegravir, bictegravir | Extremely potent with few side effects. Take separate from PPIs etc. |
Fusion inhibitor | ||
CCR5 inhibitor | ||
CD4-mAb | ibalizumab | Blocks entry of HIV into CD4 cells. |
Specific Medications
Medication | Abbr | Class | Notes |
---|---|---|---|
lamivudine | 3TC | NRTI | |
emtricitabine | FTC | NRTI | |
tenofovir disoproxol fumarate | TDF | NRTI | |
tenofovir alafenamide | TAF | NRTI | Fewer renal and bone effects. |
zidovudine | AZT | NRTI | |
abacavir | ABC | NRTI | Need to check HLA-B*5701 before starting therapy. |
efavirenz | EFZ | NNRTI | |
nevirapine | NVP | NNRTI | |
rilpivirine | RPV | NNRTI | Take with meal, not with PPI. |
doravirine | DOR | NNRTI | |
lopinavir/ritonavir | LPV/r | PI | GI side effects. |
darunivir | DRV | PI | |
dolutegravir | DTG | INSTI | Increases metformin levels. Avoid in pregnancy. |
elvitegravir/cobicistat | EVG/c | INSTI | Requires booster that has drug interaction. |
raltegravir | RAL | INSTI | First INSTI. BID dosing. Only INSTI that can be used in pregnancy. |
bictegravir | BIC | INSTI | |
cabotegravir | CAB | INSTI | Long-acting injectable available. |
ibalizumab | CD4-receptor antibody. |
Single-Tablet Regimens
Brand name | NRTIs | Non-NRTI | First-line? | Notes |
---|---|---|---|---|
Atripla | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | Older regimen. Neuropsychiatric symptoms, possibly including suicide. |
Biktarvy | tenofovir alafenamide / emtricitabine | bictegravir (INI) | Yes | |
Complera | tenofovir disoproxil fumarate / emtricitabine | rilpivirine (NNRTI) | No | Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs. |
Delstrigo | tenofovir disoproxil fumarate / lamivudine | doravirine (NNRTI) | No | |
Dovato | emtricitabine | dolutegravir (INI) | Yes | Two-medication regimen |
Genvoya | tenofovir alafenamide / emtricitabine | elvitegravir/cobicistat (INI) | See Stribild, above. | |
Odefsey | tenofovir alafenamide / emtricitabine | rilpivirine (NNRTI) | No | |
Stribild | tenofovir disoproxil fumarate / emtricitabine | elvitegravir/cobicistat (INI) | No | Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70. |
Symfi | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | |
Symtuza | tenofovir alafenamide / emtricitabine | darunavir/cobicistat (PI) | No | |
Triumeq | abacavir / lamivudine | dolutegravir (INI) | Yes | Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection. |
Considerations
- Hepatitis B: Avoid Triumeq; use TDF/FTC-based regimen instead
- CKD: Avoid Stribild in CrCl <70
Further Reading
- Andany N and Gold WL. Five things to know about single-tablet antiretroviral treatment (once daily). CMAJ. 2016;188(13)971.
- Gandhi M and Gandhi RT. Single-Pill Combination Regimens for Treatment of HIV-1 Infection. N Engl J Med. 2014;371:248-259.